Schering Corporation

Merck Sharp + Dohme Corp.

Pharmacopeia Drug Discovery, Inc.

Schering-Plough Corporation

Daniel M Solomon

Robert G Aslanian

Kevin D McCormick

Neng-Yang Shih

Stuart B Rosenblum

Wing C Tom

Michael Berlin

Pauline C Ting

John J Piwinski

Mwangi W Mutahi

James J Kaminski

Elijah H Gold

Christopher W Boyce

Henry A Vaccaro

Pietro Mangiaracina

Manuel De Lera Ruiz

Qingbei Zeng

Jianhua Cao

Steven K White

Junying Zheng

Xiaohong Zhu

Mwangi Wa Mutahi

John J Baldwin

Ashit K Ganguly

Ge Li

Ronald L Wolin

Wayne D Vaccaro

Purakkattle J Biju

Richard J Friary

Jianhua Chao

Joe F Lee

Laura S Lehman De Gaeta

David J Conn

Joseph A Kozlowski

Michael J Green

Younong Yu

Margaret H Sherlock

Yeon-Hee Lim

Wei Zhou

Andrew T Lupo

Frank J Villani

Nicholas I Carruthers

Vera A Seidl

John A Hey

Loretta A Bober

Jay S Fine

Dhiru B Vashi

Shing-Chun C Wong

James P Jakway

Michael J Grace

Tom G Wing

John C Anthes

Hongwu Yang

Yoon Joo Lee

Rema Danielle Bitar

Michael Y Berlin

Kevin D Mc Cormick

The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: 

C20-C21 substituted glucocorticoid receptor agonists

Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein Mis N; X is a bond, optionally substituted alkylene, alkenylene, &#x2014;O&#x2014;, &#x2014;CHN(R)&#x2014;, &#x2014;N(R)CH&#x2014;, &#x2014;N(R)&#x2014;, &#x2014;NHC(O)&#x2014;, &#x2014;OCH&#x2014;, &#x2014;CHO&#x2014;, or &#x2014;S(O)&#x2014;; and Y is &#x2014;(CH)&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;C(&#x2550;NOR)&#x2014; or &#x2014;SO&#x2014;;

Substituted aniline derivatives useful as histamine H3 antagonists

Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: 

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Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein:

Disclosed are novel compounds of the formula  Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a Hreceptor antagonist.

Piperidine compounds

Disclosed are novel compounds of the formula wherein Ris benzimidazolone derivative, Mand Mare optionally substituted carbon or nitrogen, Rincludes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification, and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an Hreceptor antagonist.

Disclosed are novel compounds of the formula wherein Ris optionally substituted benzimidazolyl or a derivative thereof; Ris optionally substituted aryl or heteroaryl; Mand Mare C(R) or N; and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an Hreceptor antagonist.

Benzimidazole derivatives useful as histamine H3 antagonists

Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H. receptor antagonist.

The present invention discloses novel substituted imidazole compounds which have H receptor antagonist or dual histamine-H and H receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, nasal congestion, inflammatory and CNS-related diseases and others.

Substituted imidazoles as dual histamine H1 and H3 agonists or antagonists

The present invention discloses novel substituted imidazole compounds which have dual histamine-H and H receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.

Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms

Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula I. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment. Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H, receptor antagonist.

Imidazoylalkyl substituted with a five, six or seven membered

Compounds of formula ##STR1## or pharmaceutically acceptable salts thereof, wherein E, Q, T, U, V, L, Z, X, W, M, Y and Y' are as set forth herein, are described. These compounds are useful as agents in the treatment of allergy, inflammation, autoimmune diseases, B-cell lymphomas, tumors, and the after effects of bone marrow transplantation.

Naphthyridines which affect IL-4 and G-CSF

Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl; R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH. Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.

Tricyclic derivatives, compositions and methods of use

Growing community of inventors

Edison, NJ, United States of America

Daniel M Solomon